Ritalinic Acid
(Synonyms: 利太林酸; Ritalinate) 目录号 : GC44844
An Analytical Reference Standard
Cas No.:19395-41-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ritalinic acid is an inactive, major metabolite of methylphenidate , a schedule II drug in the United States commonly used as a psychostimulant for the treatment of attention-deficit hyperactivity disorder, also known as ADHD. Ritalinic acid is reported to reach plasma concentrations of 1-2 orders of magnitude greater than that of the parent drug and has been monitored in urine to ensure compliance with treatment programs. This product is intended for forensic and biological research purposes.
| Cas No. | 19395-41-6 | SDF | |
| 别名 | 利太林酸; Ritalinate | ||
| Canonical SMILES | OC(C(C1=CC=CC=C1)C2CCCCN2)=O | ||
| 分子式 | C13H17NO2 | 分子量 | 219.3 |
| 溶解度 | Methanol: 1 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.56 mL | 22.7998 mL | 45.5996 mL |
| 5 mM | 0.912 mL | 4.56 mL | 9.1199 mL |
| 10 mM | 0.456 mL | 2.28 mL | 4.56 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Ritalinic Acid in urine: Impact of age and dose
Pract Lab Med 2021 Oct 23;27:e00258.PMID:34754895DOI:10.1016/j.plabm.2021.e00258.
Objectives: The objective of this work was to study the results of urine drug testing for Ritalinic Acid (RA), the major urinary metabolite of methylphenidate (MP) (e.g., Ritalin®). The impact of age from 4 to 65 years old and older on median levels of RA was investigated as well as potential variations in pH, specific gravity and creatinine content of the patient urine samples. Design and methods: Samples from patients who were 1) prescribed MP and found to be positive for RA, 2) prescribed MP but found to be negative for RA and 3) not prescribed MP but tested positive for RA were examined by liquid chromatography - mass spectrometry/mass spectrometry (LC-MS/MS) for RA concentration. The levels of RA were examined for median and average levels and further normalized and transformed to reveal a near gaussian distribution. Results: Over 20,000 samples from patients who were prescribed MP were examined for this work. Analysis of these data for a subset of patients prescribed MP and testing positive for RA revealed statistically different median values of RA for school age patients of 6 years old through 17 years old from adult patients 18 through 64 years old. Another 6751 samples were positive for RA without a prescription but were not included in the overall assessment of these data. Conclusions: While not clear as to the reason, these data indicate that school age children under the age of 18 have much higher levels of RA than adult patients. These results can be used to estimate "normal" levels of RA in these chronically dosed populations.
Biotransformation of Ritalinic Acid by laccase in the presence of mediator TEMPO
N Biotechnol 2018 Jul 25;43:44-52.PMID:28855123DOI:10.1016/j.nbt.2017.08.008.
Methylphenidate is widely used as a medication for the treatment of attention deficit hyperactivity disorder (ADHD) in children. Less than 1% of methylphenidate is excreted unchanged in urine, while 80% of an oral dose is excreted as Ritalinic Acid (which is reportedly poorly degradable). This study aims to investigate the biotransformation of Ritalinic Acid by free and immobilized enzymes. The influence of various laccase mediators on biotransformation efficiency has been tested. Formation of the main transformation products has been monitored and their potential structures suggested. The effective transformation of Ritalinic Acid was observed only in the presence of 2,2,6,6-tetramethylpiperidine 1-oxyl mediator (TEMPO). The most effective enzyme was the laccase of T. versicolor 159. The main transformation product was an N-methyl derivative of Ritalinic Acid. Ritalinic Acid was also reduced to aldehyde and alcohol, and a broad spectrum of intermediate complexes with oxoammonium ion of TEMPO were detected. This is the first time the biotransformation of Ritalinic Acid has been investigated in detail.
The Pharmacokinetics and Pharmacogenomics of Psychostimulants
Child Adolesc Psychiatr Clin N Am 2022 Jul;31(3):393-416.PMID:35697392DOI:10.1016/j.chc.2022.03.003.
The psychostimulants-amphetamine and methylphenidate-have been in clinical use for well more than 60 years. In general, both stimulants are rapidly absorbed with relatively poor bioavailability and short half-lives. The pharmacokinetics of both stimulants are generally linear and dose proportional although substantial interindividual variability in pharmacokinetics is in evidence. Amphetamine (AMP) is highly metabolized by several oxidative enzymes forming multiple metabolites while methylphenidate (MPH) is primarily metabolized by hydrolysis to the inactive metabolite Ritalinic Acid. At present, pharmacogenomic testing as an aid to guide dosing and personalized treatment cannot be recommended for either agent. Few pharmacokinetically based drug-drug interactions (DDIs) have been documented for either stimulant.
Bacterial isolates degrading ritalinic acid-human metabolite of neuro enhancer methylphenidate
N Biotechnol 2018 Jul 25;43:30-36.PMID:28855122DOI:10.1016/j.nbt.2017.08.009.
The consumption of nootropic drugs has increased tremendously in the last decade, though the studies on their environmental fate are still scarce. Nootropics are bioactive compounds designed to alter human's physiology therefore the adverse effects towards wildlife can be expected. In order to understand their environmental impact, the knowledge on their transformation pathways is necessary. Methylphenidate belongs to the most prescribed neuro-enhancers and is among the most favored smart drugs used in non-medical situations. It is metabolized in human liver and excreted as Ritalinic Acid. Here, we showed for the first time that Ritalinic Acid can be biodegraded and used as a sole carbon and nitrogen source by various microbial strains originating from different environmental samples. Five axenic strains were isolated and identified as: Arthrobacter sp. strain MW1, MW2 and MW3, Phycicoccus sp. strain MW4 and Nocardioides sp. strain MW5. Our research provides the first insight into the metabolism of Ritalinic Acid and suggests that it may differ depending on the strain and growth conditions, especially on availability of nitrogen. The isolates obtained in this study can serve as model organisms in further studies on the catabolism of Ritalinic Acid and methylphenidate but potentially also other compounds with similar structures. Our findings have important implication for the sewage epidemiology. We demonstrated that Ritalinic Acid is subject to quick and efficient biodegradation thus its use as a stable biomarker should be reconsidered.
Ritalinic Acid Stimulates Human Sperm Motility and Maintains Vitality In Vitro
World J Mens Health 2020 Jan;38(1):61-67.PMID:31081298DOI:10.5534/wjmh.180127.
Purpose: To evaluate the in vitro impact of Ritalinic Acid (RA), a major metabolite of methylphenidate (drug to treat attention-deficit hyperactivity disorder), on sperm motility, vitality and oxidative stress. Materials and methods: Semen samples (n=13) were collected from healthy donors and a semen analysis was performed according to World Health Organization. Density gradient centrifugation was performed to isolate motile sperm. Samples were incubated with different concentrations (0, 1, 10, 100, and 1,000 ng/mL) of RA. The non-exposed group (0 ng/mL) was defined as the control group. Samples were analyzed for motility at different time points (0, 60, 150, 240, and 300 minutes) and for vitality and oxidation reduction potential (ORP) (at 0, 240, and 300 minutes). Sperm motility was assessed manually and motion kinetic parameters were recorded by computer aided semen analysis. Results: RA at any tested concentration significantly increased sperm motility compared to the control in a time-dependent manner with a maximum increase after 240 minutes. Motion kinetic parameters were not comparable. For sperm vitality, supplementation with RA significantly maintained survival at higher levels, while non-treated sperm gradually died. These higher levels of vitality were maintained with rising RA concentrations of up to 1,000 ng/mL. A non-significant trend of increased ORP was observed in all study groups. Conclusions: RA increases sperm motility and maintains vitality at any concentration tested. Therefore, RA might be utilized to improve sperm quality in asthenozoospermic specimens. However, further investigation is ongoing to evaluate the effect of RA on other sperm parameters.